Recent Applications of Diversity-Oriented Synthesis Toward Novel, 3-Dimensional Fragment Collections
نویسندگان
چکیده
منابع مشابه
Diversity-Oriented Synthesis-Facilitated Medicinal Chemistry: Toward the Development of Novel Antimalarial Agents
Here, we describe medicinal chemistry that was accelerated by a diversity-oriented synthesis (DOS) pathway, and in vivo studies of our previously reported macrocyclic antimalarial agent that derived from the synthetic pathway. Structure-activity relationships that focused on both appendage and skeletal features yielded a nanomolar inhibitor of P. falciparum asexual blood-stage growth with impro...
متن کاملRecent advances in multicomponent reactions for diversity-oriented synthesis.
Interest in multicomponent reactions (MCRs) has surged during the past two decades as interest in the efficient synthesis of small molecule libraries has gained prominence. MCRs fill an important niche in library synthesis by providing direct access to library compounds and by serving as starting points for Diversity-Oriented Synthesis (DOS). Recent advances in the area of MCR chemistry have in...
متن کاملRecent Applications of Meldrum's Acid in Organic Synthesis
Reactions of Meldrum's acid and its derivatives in view of their application in synthesis of diaminofurans,ketenimines, amidoesters, triamides, and diionic compounds, observed during the last decade in our laboratory,are reviewed.
متن کاملRoute to three-dimensional fragments using diversity-oriented synthesis.
Fragment-based drug discovery (FBDD) has proven to be an effective means of producing high-quality chemical ligands as starting points for drug-discovery pursuits. The increasing number of clinical candidate drugs developed using FBDD approaches is a testament of the efficacy of this approach. The success of fragment-based methods is highly dependent on the identity of the fragment library used...
متن کاملPseudo-Five-Component Condensation for the Diversity-Oriented Synthesis of Novel Indoles and Quinolines Containing Pseudo-Peptides (Tricarboxamides)
A novel series of indole and quinoline tricarboxamides were synthesized using simple and efficient one-pot pseudo-five-component reactions of 2-formylindole or 2-chloro-3-formyl quinolines, isocyanides, amines, and Meldrum’s acid as a CH-acid in CH2Cl2 at room temperature. This conversion has been achieved via the construction of new bonds including two C-C bonds, two ...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Frontiers in Chemistry
سال: 2018
ISSN: 2296-2646
DOI: 10.3389/fchem.2018.00460